间二三氟甲苯置于[ir(Cod)(Ome)]2 Sodium Periodate,4,4'-二叔丁基-2,2'-二吡啶体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 20.25H,反应生成 3,5-双(三氟甲基)苯硼酸 参考文献:One-Pot Synthesis Of Arylboronic Acids And Aryl Trifluoroborates By Ir-Catalyzed Borylation Of Arenes 标题:One-Pot Synthesis Of Arylboronic Acids And Aryl Trifluoroborates By Ir-Catalyzed Borylation Of Arenes 摘要:The Synthesis Of Arylboronic Acids And Aryl Trifluoroborates In A One-Pot Sequence By Ir-Catalyzed Borylation Of Arenes Is Reported. To Prepare The Arylboronic Acids,The Ir-Catalyzed Borylation Is Followed By Oxidative Cleavage Of The Boronic Ester With Naio4. To Prepare The Aryltrifluoroborate,The Ir-Catalyzed Borylation Is Followed By Displacement Of Pinacol By Khf2. These Two-Step Sequences Give Products That Are More Reactive Toward Subsequent Chemistry Than The Initially Formed Pinacol Boronates. DOI:10.1021/ol062903O
专利号:US-9428524-B2 优先权日:2010-05-25 标 题:Synthetic process for the manufacture of ecteinascidin compounds 发明人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN 权利人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN; PHARMA MAR SA 摘要:This invention relates to compounds of formula II: wherein R 1 , R 2 , Prot SH , and Prot NH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
专利号:US-7470795-B2 优先权日:2004-07-27 标 题:Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides 发明人:WANG XIAO-JUN; WIRTH THOMAS; NICOLA THOMAS; ZHANG LI; FRUTOS ROGELIO PEREZ; XU YIBO; KRISHNAMURTHY DHILEEPKUMAR; NUMMY LAURENCE JOHN; VARSOLONA RICHARD J; SENANAYAKE CHRIS HUGH; KROEBER JUTTA; REEVES DIANA 权利人:BOEHRINGER INGELHEIM PHARMA; BOEHRINGER INGELHEIM INT 摘要:Disclosed is a multi-step process for preparing a compound of Formula I: n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “a†, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
专利号:US-2008227851-A1 优先权日:2007-03-12 标题 :Laulimalide and laulimalide analogs 发明人:WENDER PAUL A 权利人:WENDER PAUL A 摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
专利号:US-2009088571-A1 优先权日:2004-07-27 标题 :Synthesis of 6,7-Dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
专利号:EP-2107067-A1 优先权日:2008-04-03 标 题 :Boron catalysed peptide synthesis 发明人:QUAEDFLIEG PETER JAN LEONARD MARIO; NUIJENS TIMO; VRIES DE JOHANNES GERARDUS; KALKEREN VAN HENRI ANTONIUS 权利人:DSM IP ASSETS BV 摘要:The invention relates to a method of synthesising a dipeptide, an oligopeptide or polypeptide comprising coupling a first amino acid or peptide to a second amino acid or peptide in the presence of a boron compound comprising a boron oxygen bond, which boron compound catalyses the formation of a peptidic bond, wherein one of the stereoisomers is formed in excess of the other stereoisomer or stereoisomers.
[参考文献]: F Adebodun, Et Al. Multinuclear Magnetic Resonance Studies On Serine Protease Transition State Analogues. J Cell Biochem. 1989 Jun;40(2):249-60.
合成参考文献
摘要:Sartori, G.; Maggi, R., Science of Synthesis, (2010) 47, 520. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 197. 摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 346. 摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2018) 4, 128. 摘要:Kubik, S., Science of Synthesis Knowledge Updates, (2013) 3, 265.